Synthesis of 4′-epi-iodo-4′-deoxy-daunorubicin, a potential cancer radiotherapeutic agent

被引：5

作者：

Murali, D ^{[1
]}

DeJesus, OT ^{[1
]}

机构：

[1] Univ Wisconsin, Sch Med, Dept Phys Med, Madison, WI 53706 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(98)00616-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have prepared 4'-epi-iodo-4'-deoxy-daunorubicin (IDDNR)(1), a doxorubicin analog, via a 5-step synthesis involving a protected daunorubicin triflate derivative (4). This triflate derivative will allow the facile and regiospecific nucleophilic preparation of I-125 or Br-80m labelled analogs of IDDNR. Auger electron-emitting I-125- or Br-80m-labelled analogs of IDDNR may have potential as cancer radiotherapeutic agents. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3419 / 3422

页数：4

共 16 条

[1]

Bloomer W D, 1978, Pathobiol Annu, V8, P407

[2] SPECIFIC CYTO-TOXICITY OF 16-ALPHA-[I-125]IODESTRADIOL FOR ESTROGEN RECEPTOR-CONTAINING BREAST-CANCER CELLS [J].

BRONZERT, DA ;

HOCHBERG, RB ;

LIPPMAN, ME .

ENDOCRINOLOGY, 1982, 110 (06) :2177-2179

[3] RADIOTOXICITY OF I-125 IN MAMMALIAN-CELLS .2. COMPARATIVE-STUDY ON CELL SURVIVAL AND CYTOGENETIC RESPONSES TO UDR-I-125, 131IUDR, AND TDR1-H-3 [J].

CHAN, PC ;

LISCO, E ;

LISCO, H ;

ADELSTEIN, SJ .

RADIATION RESEARCH, 1976, 67 (02) :332-343

[4]

DESOMBRE ER, 1988, CANCER RES, V48, P899

[5]

DESOMBRE ER, 1988, CANCER RES, V48, P5805

[6]

FORMELLI F, 1987, CANCER RES, V47, P5401

[7] [125I/127I/131I] iodorhodamine:: Synthesis, cellular localization, and biodistribution in athymic mice bearing human tumor xenografts and comparison with [99mTc]Hexakis(2-methoxyisobutylisonitrile) [J].

Harapanhalli, RS ;

Roy, AM ;

Adelstein, SJ ;

Kassis, AI .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (12) :2111-2117

[8] Anthracyclines in the treatment of cancer - An overview [J].

Hortobagyi, GN .

DRUGS, 1997, 54 (Suppl 4) :1-7

[9]

Mariani G, 1996, J NUCL MED, V37, pS22

[10] INDUCTION OF DOUBLE-STRANDED BREAKS IN DNA BY BINDING WITH AN I-125-LABELED ACRIDINE [J].

MARTIN, RF .

INTERNATIONAL JOURNAL OF RADIATION BIOLOGY, 1977, 32 (05) :491-497

← 1 2 →